中文名：ICI-118551盐酸盐
英文名：ICI-118551 Hydrochloride
纯度：≥98%
货号：I413910
Cas号：1217094-53-5
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
ICI-118551 is a highly selectiveβ2-adrenergic receptor antagonistwithKivalues of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.
Targets
β2-adrenergic receptor (Cell-free assay); β1-adrenergic receptor (Cell-free assay); β3-adrenoceptor (Cell-free assay) 0.7nM(Ki); 49.5nM(Ki); 611nM(Ki)
In vitro
ICI-118551 inhibits cAMP accumulation by 50% (IC50 = 1.7 mM). Pharmacological experiments proves that the right shift of the norepinephrine dose-response curve by ICI 118551 is mediated via a beta(2)-adrenoceptor/G(i/o) protein-dependent pathway enhancing NO production in the endothelium; these results are corroborated in beta-adrenoceptor and endothelial NO synthase knockout mice where ICI 118551 has no effect. ICI 118551 increases vascular lumen diameter in lung sections and reduces pulmonary arterial pressure under normoxia and under hypoxia in the isolated perfused lung model. Transgenic mice with high beta(2)AR number and increased G(i) levels have normal basal contractility but show a similar negative inotropic response to ICI 118,551. Overexpression of human beta(2)AR in rabbit myocytes using adenovirus potentiates the negative inotropic effect of ICI 118,551. In human, rabbit, and mouse myocytes, the negative inotropic effects are blocked after treatment of cells with pertussis toxin to inactivate G(i), and overexpression of G(i)alpha(2) induces the effect de novo in normal rat myocytes.
In vivo
After 1 week of treatment, ICI 118,551 has no effect on the beta 1-receptor mediated shortening of electromechanical systole (QS2I), the rise in systolic pressure and rise in renin, whereas these responses are blocked by a dose factor of eight after propranolol. ICI 118,551 and propranolol equally block the beta 2-receptor mediated fall in diastolic pressure and the rise in noradrenaline. beta 2-selective blockade by ICI 118,551 lowers blood pressure.
Cell Research(from reference)
Cell lines：MEF cell line
Concentrations：10μM
Incubation Time：2-hours incubation at room-temperature
查看阿拉丁官网此产品相关对应页面：https://www.aladdin-e.com/zh_cn/I413910.html
关键字： ICI-118,5512-?Butanol,1-?[(2,?3-?dihydro-?7-?methyl-?1H-?inden-?4-?yl)?oxy]?-?3-?[(1-?methylethyl)?amino]?-?,hydrochloride (1:1)
上海阿拉丁生化科技股份有限公司是A股上市公司（（股票代码：688179），专注于科研试剂的研发、生产和销售，已陆续建立多个工厂和研发中心。作为领军企业，阿拉丁始终坚持质量第一，连续13年被评为“最受欢迎试剂品牌”。
阿拉丁目前常备库存试剂产品品种超过7万种，SKU总数超过46万，产品线涵盖了化学试剂、生化试剂、药靶配体、蛋白质和抗体等多个领域，是国内少数化学试剂到生物试剂全面发展的国产试剂品牌，产品同步发布在我们国内外电商平台。